Preparation method for prednisolone

Abstract

The invention discloses a preparation method for prednisolone. According to the method, a compound as shown in a formula 1 is used as a starting material and is successively subjected to biological conversion, oxidation, esterification, reduction and hydrolysis so as to obtain prednisolone. The preparation method has the advantages of easy availability of the starting material, simple process route, no use of expensive auxiliary materials, high yield, and capacity of effectively overcoming the technical problems of long process routes, low yield, a great number of by-products, high cost, unfriendliness to environment and the like in conventional preparation methods for prednisolone.

Description

technical field [0001] The invention relates to a preparation method of steroidal compounds, in particular to the preparation of prednisolone, and belongs to the technical field of pharmacy. Background technique [0002] Prednisolone belongs to adrenal glucocorticoid drugs, which has various pharmacological effects such as anti-inflammation, anti-allergy and immune suppression. It is mainly used for severe bacterial infections and severe allergic diseases, various thrombocytopenic purpura, granulocytic Reduction syndrome, severe skin disease, immune rejection of organ transplantation, tumor treatment and ocular inflammation sensitive to glucocorticoids, etc. [0003] The preparation method of prednisolone mainly contains following several at present: [0004] Method 1: Using hydrocortisone as the starting material, using Arthrobacter simplex for biological dehydrogenation. The conversion rate of this method is relatively low, generally no more than 80%. For example, see Sc...

AI Technical Summary

Problems solved by technology

Although this route is widely used, due to the selective protection of ketone carbonyl in the reaction process, and the by-products are not easy to separate, the yield and purity of the product are seriously affected;

[0006] Method 3: Patents CN101397324A and CN103387595A both use 17α-hydroxy-1,4,9-triene-pregna-3,20-dione as the starting substrate, and undergo modifications at positions 9, 11 and 21 to obtain prednisone Long, but its 11-position β-hydroxyl is introduced by the reaction of bromo-hydroxyl, and it needs to be debrominated with a reducing agent such as chromium salt, and the operation is complicated

[0007] Method 4: Patent CN105801650A uses dihydroxyprogesterone dehydrogenation as a raw material, first transforms the α-hydroxyl at the 11th position into a β-hydroxyl, and then obtains prednisolone through reactions such as iodination and replacement. There are many steps and the operation is difficult , not conducive to mass production

Images